Non-invasive assessment of inter-and intrapatient variability of integrin expression in metastasized prostate cancer by PET.

Purpose: Due to the high expression of the integrin αvβ3 not only on endothelial cells, but also on mature osteoclasts and prostate cancer cells, imaging of osseous metastases with αvβ3-targeted tracers seems promising. However, little is known about the patterns of αvβ3-expression in metastasized prostate cancer lesions in-vivo. Thus we evaluated the uptake of the αvβ3-specific PET tracer [18F]Galacto-RGD for assessment of bone metastases in prostate cancer patients.

18F-labeled galacto and PEGylated RGD dimers for PET imaging of αvβ3 integrin expression.

Purpose: In vivo imaging of α(v)β(3) has important diagnostic and therapeutic applications. (18)F-Galacto-arginine-glycine-aspartic acid (RGD) has been developed for positron emission tomography (PET) imaging of integrin α(v)β(3) expression and is now being tested on humans. Dimerization and multimerization of cyclic RGD peptides have been reported to improve the integrin α(v)β(3)-binding affinity due to the polyvalency effect.

Assessment of alphavbeta3 integrin expression after myocardial infarction by positron emission tomography.

Aims: The purpose of this study was to determine the feasibility of a new positron emission tomography (PET) imaging approach using an (18)F-labelled alpha(v)beta(3) integrin antagonist ((18)F-Galacto-RGD) to monitor the integrin expression after myocardial infarction.

Methods And Results: Male Wister rats were subjected to 20 min transient left coronary artery occlusion followed by reperfusion. Autoradiographic analysis and in vivo PET imaging were used to determine myocardial (18)F-Galacto-RGD uptake at different time points following reperfusion.

Patterns of alphavbeta3 expression in primary and metastatic human breast cancer as shown by 18F-Galacto-RGD PET.

Unlabelled: The integrin alpha(v)beta(3) is a key player in angiogenesis and metastasis. Our aim was to study the uptake patterns of the alpha(v)beta(3)-selective PET tracer (18)F-galacto-RGD in invasive ductal breast cancer.

Methods: Sixteen patients with primary (n = 12) or metastasized breast cancer (n = 4) were examined with (18)F-galacto-RGD PET.

Comparison of integrin alphaVbeta3 expression and glucose metabolism in primary and metastatic lesions in cancer patients: a PET study using 18F-galacto-RGD and 18F-FDG.

Unlabelled: The expression of alpha(v)beta(3) and glucose metabolism are upregulated in many malignant lesions, and both are known to correlate with an aggressive phenotype. We evaluated whether assessment of alpha(v)beta(3) expression and of glucose metabolism with PET using (18)F-galacto-RGD and (18)F-FDG provides complementary information in cancer patients.

Methods: Eighteen patients with primary or metastatic cancer (non-small cell lung cancer [NSCLC], n = 10; renal cell carcinoma, n = 2; rectal cancer, n = 2; others, n = 4) were examined with PET using (18)F-galacto-RGD and (18)F-FDG.

[18F]galacto-RGD positron emission tomography for imaging of alphavbeta3 expression on the neovasculature in patients with squamous cell carcinoma of the head and neck.

Purpose: [(18)F]Galacto-RGD has been developed for positron emission tomography (PET)-imaging of alphavbeta3 expression, a receptor involved in angiogenesis and metastasis. Our aim was to study the feasibility of PET imaging with [(18)F]Galacto-RGD in patients with squamous cell carcinoma of the head and neck (SCCHN).

Experimental Design: Eleven patients with primary diagnosis of SCCHN were examined.

Evaluation of cardiac beta-adrenoreceptors in the isolated perfused rat heart using (S)-11C-CGP12388.

Unlabelled: (S)-(11)C-CGP12388 ((11)C-CGP12388) was recently developed as an in vivo PET tracer for the evaluation of cardiac beta-adrenergic receptors. The purpose of this study was to evaluate the myocardial kinetics of (11)C-CGP12388 using the perfused rat heart model.

Methods: Normal rat hearts were cannulated for retrograde perfusion according to the Langendorff method.

PET imaging with [11C]methyl- L-methionine for therapy monitoring in patients with rectal cancer.

In this study we evaluated whether positron emission tomography (PET) using the amino acid [11C]methyl- L-methionine (MET) may be used for therapy monitoring in patients with rectal cancer who are undergoing preoperative chemoradiotherapy. A total of 41 MET-PET scans were performed in 26 patients with locally advanced rectal cancers. All patients were examined prior to chemoradiotherapy.